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Bioorg Med Chem ; 105: 117736, 2024 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-38677111

RESUMEN

Leishmaniasis and Chagas disease are neglected tropical diseases caused by Trypanosomatidae parasites. Given the numerous limitations associated with current treatments, such as extended treatment duration, variable efficacy, and severe side effects, there is an urgent imperative to explore novel therapeutic options. This study details the early stages of hit-to-lead optimization for a benzenesulfonyl derivative, denoted as initial hit, against Trypanossoma cruzi (T. cruzi), Leishmania infantum (L. infantum) and Leishmania braziliensis (L. braziliensis). We investigated structure - activity relationships using a series of 26 newly designed derivatives, ultimately yielding potential lead candidates with potent low-micromolar and sub-micromolar activities against T. cruzi and Leishmania spp, respectively, and low in vitro cytotoxicity against mammalian cells. These discoveries emphasize the significant promise of this chemical class in the fight against Chagas disease and leishmaniasis.


Asunto(s)
Diseño de Fármacos , Leishmania infantum , Pruebas de Sensibilidad Parasitaria , Trypanosoma cruzi , Trypanosoma cruzi/efectos de los fármacos , Leishmania infantum/efectos de los fármacos , Relación Estructura-Actividad , Estructura Molecular , Tripanocidas/farmacología , Tripanocidas/síntesis química , Tripanocidas/química , Relación Dosis-Respuesta a Droga , Antiprotozoarios/farmacología , Antiprotozoarios/síntesis química , Antiprotozoarios/química , Humanos , Animales , Sulfonas/farmacología , Sulfonas/síntesis química , Sulfonas/química
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